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Targeted Protein Degrader
A modular platform, so the first degrader is a matter of weeks rather than months.
Where a degrader program loses time
A degrader is three parts — a target protein ligand, a linker and an E3 ligase ligand — and the first campaign usually spends its time making the parts rather than testing the combinations.
We have worked on all three since 2016, which means most of the parts already exist.
The platform
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A modular system
More than 1,000 of the most frequently used linkers — PEG, alkyl, clickable, rigid and others — are available through WuXi AppTec LabNetwork, as are more than 200 common E3 ligase ligands including VHL and CRBN.
Customized degraders are made from milligram to kilogram scale on the same platform.
A target protein ligand series already coupled to a linker set is usually the difference between a first degrader in six weeks and one in six months.
Molecular glues
Degradation without a linker, where a small molecule stabilizes a new interface between an E3 ligase and the target. The design and screening work draws on the same E3 ligase ligand collection and degrader chemistry as the linker-based programs, so both approaches can be run on a target while it is still open which one will work.
Analysis and testing
An innovative online dilution system designed for targeted protein degraders, native mass spectrometry for ternary complex confirmation, and proteomics studies to identify off-target effects.
Comprehensive in vitro and in vivo testing is run by the WuXi DMPK team.